ZA200705472B - [4-(heteroaryl) piperazin-1-yl]-(2,5-substituted-phenyl) methanone derivatives as glycine transporter 1 (GlyT-1) inhibitors for the treatment of neurological and neuropsychiatric disorders - Google Patents

[4-(heteroaryl) piperazin-1-yl]-(2,5-substituted-phenyl) methanone derivatives as glycine transporter 1 (GlyT-1) inhibitors for the treatment of neurological and neuropsychiatric disorders

Info

Publication number
ZA200705472B
ZA200705472B ZA200705472A ZA200705472A ZA200705472B ZA 200705472 B ZA200705472 B ZA 200705472B ZA 200705472 A ZA200705472 A ZA 200705472A ZA 200705472 A ZA200705472 A ZA 200705472A ZA 200705472 B ZA200705472 B ZA 200705472B
Authority
ZA
South Africa
Prior art keywords
glyt
piperazin
neurological
heteroaryl
inhibitors
Prior art date
Application number
ZA200705472A
Other languages
English (en)
Inventor
Jolidon Synese
Norcross Roger David
Narquizian Robert
Pinard Emmanuel
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of ZA200705472B publication Critical patent/ZA200705472B/xx

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/081,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/433Thidiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38Nitrogen atoms
    • C07D277/42Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D285/00Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/121,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
    • C07D285/1251,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
    • C07D285/135Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
ZA200705472A 2005-01-07 2007-07-04 [4-(heteroaryl) piperazin-1-yl]-(2,5-substituted-phenyl) methanone derivatives as glycine transporter 1 (GlyT-1) inhibitors for the treatment of neurological and neuropsychiatric disorders ZA200705472B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP05100077 2005-01-07

Publications (1)

Publication Number Publication Date
ZA200705472B true ZA200705472B (en) 2008-09-25

Family

ID=35998949

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200705472A ZA200705472B (en) 2005-01-07 2007-07-04 [4-(heteroaryl) piperazin-1-yl]-(2,5-substituted-phenyl) methanone derivatives as glycine transporter 1 (GlyT-1) inhibitors for the treatment of neurological and neuropsychiatric disorders

Country Status (19)

Country Link
US (1) US7220744B2 (xx)
EP (1) EP1838308B1 (xx)
JP (1) JP5006799B2 (xx)
KR (1) KR100895752B1 (xx)
CN (1) CN101137363B (xx)
AR (1) AR052866A1 (xx)
AT (1) ATE472327T1 (xx)
AU (1) AU2005324024B2 (xx)
BR (1) BRPI0519794A2 (xx)
CA (1) CA2593463C (xx)
DE (1) DE602005022113D1 (xx)
ES (1) ES2346335T3 (xx)
IL (1) IL184353A (xx)
MX (1) MX2007008189A (xx)
NO (1) NO20073667L (xx)
RU (1) RU2396270C2 (xx)
TW (1) TWI313174B (xx)
WO (1) WO2006072436A1 (xx)
ZA (1) ZA200705472B (xx)

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AR051091A1 (es) * 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
CN101083982A (zh) * 2004-09-20 2007-12-05 泽农医药公司 用于治疗硬脂酰CoA去饱和酶介导的疾病的杂环衍生物
AU2005329423A1 (en) 2004-09-20 2006-09-28 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
WO2006034441A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
JP5080256B2 (ja) * 2004-09-20 2012-11-21 ゼノン・ファーマシューティカルズ・インコーポレイテッド 二環式複素環誘導体およびステアロイル−CoAデサチュラーゼ(SCD)のインヒビターとしてのそれらの使用
MX2007015216A (es) 2005-06-03 2008-02-22 Xenon Pharmaceuticals Inc Derivados de aminotiazol y sus usos como agentes terapeuticos.
KR101143073B1 (ko) 2007-03-05 2012-05-08 에프. 호프만-라 로슈 아게 Glyt-1 억제제의 합성 방법
JP2012505173A (ja) 2008-10-09 2012-03-01 エフ.ホフマン−ラ ロシュ アーゲー ピロリジンn−ベンジル誘導体
TW201127806A (en) * 2009-09-02 2011-08-16 Du Pont Process for the synthesis of fluorinated ethers of aromatic acids
TW201127805A (en) * 2009-09-02 2011-08-16 Du Pont Process for the synthesis of fluorinated ethers of aromatic acids
CN101885708B (zh) * 2010-07-07 2013-03-06 中国科学院上海有机化学研究所 5-多氟烷基取代的2-氨基噻唑类化合物、合成方法及其应用
WO2011082660A1 (zh) * 2010-01-08 2011-07-14 中国科学院上海有机化学研究所 5-多氟烷基取代的2-氨基噻唑类化合物、合成方法及其应用
AU2011261375B2 (en) * 2010-06-04 2016-09-22 Albany Molecular Research, Inc. Glycine transporter-1 inhibitors, methods of making them, and uses thereof
US9012489B2 (en) * 2011-08-03 2015-04-21 Boehringer Ingelheim International Gmbh Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament
US9266838B2 (en) 2011-08-15 2016-02-23 University Of Utah Research Foundation Substituted (E)-N′-(1-phenylethylidene)benzohydrazide analogs as histone demethylase inhibitors
CA2841037C (en) * 2011-08-17 2020-03-31 Remynd Nv Piperazine thiazole derivatives useful in the treatment of tauopathies such as alzheimer's disease
CN104119343A (zh) * 2013-04-25 2014-10-29 苏州科捷生物医药有限公司 2-三氟甲基噻二唑类化合物及其用途
KR102288648B1 (ko) * 2013-06-19 2021-08-12 유니버시티 오브 유타 리서치 파운데이션 히스톤 데메틸라제 억제제로서의 치환된 (e)-n′-(1-페닐에틸리덴)벤조하이드라지드 동족체
EP3134406A1 (en) 2014-04-24 2017-03-01 Dart Neuroscience (Cayman) Ltd Substituted 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole and 4,5,6,7-tetrahydro-2h-pyrazolo [4,3-c]pyridine compounds as glyt1 inhibitors
EP3215500A1 (en) 2014-11-05 2017-09-13 Dart NeuroScience (Cayman) Ltd. Substituted azetidinyl compounds as glyt1 inhibitors
CN105712952B (zh) * 2014-12-22 2021-03-26 上海翰森生物医药科技有限公司 2-取代氧基-5-甲砜基苯基哌嗪酰胺类似物及其制备方法和用途
CN105712945B (zh) * 2014-12-22 2020-12-01 上海翰森生物医药科技有限公司 2-取代氧基-5-甲砜基芳基哌嗪酰胺类似物及其制备方法和用途
CN117777121A (zh) 2016-10-24 2024-03-29 詹森药业有限公司 化合物及其用途
EP3700934A4 (en) 2017-10-24 2021-10-27 Yumanity Therapeutics, Inc. COMPOUNDS AND USES OF THESE COMPOUNDS
JP2022531932A (ja) 2019-05-10 2022-07-12 デシフェラ・ファーマシューティカルズ,エルエルシー ヘテロアリールアミノピリミジンアミドオートファジー阻害剤およびその使用方法
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Also Published As

Publication number Publication date
CN101137363B (zh) 2010-09-15
DE602005022113D1 (de) 2010-08-12
AU2005324024A1 (en) 2006-07-13
JP2008526796A (ja) 2008-07-24
MX2007008189A (es) 2007-08-07
RU2396270C2 (ru) 2010-08-10
AR052866A1 (es) 2007-04-11
BRPI0519794A2 (pt) 2009-03-17
EP1838308A1 (en) 2007-10-03
IL184353A0 (en) 2007-10-31
JP5006799B2 (ja) 2012-08-22
CN101137363A (zh) 2008-03-05
WO2006072436A1 (en) 2006-07-13
NO20073667L (no) 2007-07-24
US20060167009A1 (en) 2006-07-27
ATE472327T1 (de) 2010-07-15
CA2593463C (en) 2013-10-08
AU2005324024B2 (en) 2011-02-17
KR100895752B1 (ko) 2009-04-30
EP1838308B1 (en) 2010-06-30
IL184353A (en) 2012-06-28
US7220744B2 (en) 2007-05-22
ES2346335T3 (es) 2010-10-14
KR20070092759A (ko) 2007-09-13
TW200635585A (en) 2006-10-16
CA2593463A1 (en) 2006-07-13
RU2007124545A (ru) 2009-02-20
TWI313174B (en) 2009-08-11

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